Parameters of deltorphin II-mediated desensitization of hDOR and hDOR(S363A) calculated using the operational model
Parameters of the operational model (eq. 1) (Em = operational maximum; τcontrol, τdel-wt, and τdel-S363A are operational efficacies for untreated cells and deltorphin II pretreated hDOR/CHO or hDOR(S363A)/CHO cells, respectively; KA = dissociation constant) were calculated by fitting the dose response curves of stimulation of GTPγ [35S] binding or inhibition of cAMP production.
Em | τcontrol | τdel-wt | τdel-S363A | KA | |
|---|---|---|---|---|---|
| % | nM | ||||
| GTPγ[35S] | 110 ± 4 | 13 ± 5 | 1.9 ± 0.5 | 10 ± 4 | 97 ± 33 |
| cAMP | 107 ± 7 | 19 ± 18 | 3.6 ± 2.3 | 16 ± 15 | 36 ± 30 |